摘要
目的优化芥子碱皮肤与血液体外微透析方法的条件,建立芥子碱在体微透析方法。方法以芥子碱稳定性为指标,选择灌流液;采用增量法和减量法考察体积流量和质量浓度对皮肤和血液探针体外回收率的影响,确定芥子碱微透析的体积流量及取样间隔;以确定的体外微透析方法,研究芥子碱穴位及非穴位皮肤、血液在体回收率的稳定性。结果以10%乙醇/生理盐水溶液(pH=5.5)为灌流液;增量法和减量法中皮肤探针体外回收率在1～4μL/min体积流量下均相近,且皮肤与血液探针体外回收率在1.32～20.00μg/mL内与芥子碱溶液的质量浓度无关;以体积流量2μL/min,取样间隔30 min,增量法和减量法测得皮肤探针的体外回收率分别为(37.68±1.05)%和(42.85±2.82)%,血液探针分别为(78.31±2.35)%和(75.23±1.14)%;穴位皮肤、非穴位皮肤、血液在体微透析8 h,芥子碱体内回收率稳定,分别为(24.02±4.44)%、(26.51±7.67)%和(33.73±2.72)%。结论建立的芥子碱皮肤与血液微透析方法可用于白芥子涂方穴位与非穴位给药后芥子碱皮肤和血液的药代动力学研究。
AIM To investigate subcutaneous and blood microdialysis of sinapine in vitro and in vivo.METHODS Different physiological solutions were used for studying a suitable perfusate.Probe microdialysis recoveries were investigated by gain and loss method using five different drug concentrations（1.32-20.00 μg/mL） at four flow rates（1-4 μL/min） in vitro.Probe recoveries were studied under the condition of probe surgically implanted into guinea pig skin at Feishu acupoint,non-Feishu acupoint and jugular vein at the time of 8 h by loss method.RESULTS 10% ethanol / normal saline（pH=5.5） was chosen for microdialysis perfusate.In vitro recovery of sinapine determined by gain and loss method decreased as the flow rate increased.The concentration had no obvious effect on probe microdialysis recoveries.In vitro the average recoveries of subcutaneous microdialysis probes determined by gain and loss method,at flow rate of 2 μL/min,were（37.68±1.05）% and（42.85±2.82）%,respectively.The mean recoveries of blood microdialysis probes were（78.31±2.35）% and（75.23±1.14）%,respectively.The average recoveries of Feishu acupoint,non-Feishu acupoint subcutaneous and blood microdialysis probes were（24.02±4.44）%,（26.51±7.67）% and（33.73±2.72）% within 8 hours in vivo.CONCLUSION Subcutaneous and blood microdialysis of sinapine can be used for sinapine percutaneous absorption and blood pharmacokinetic studies of Baijiezi extract through guinea pig Feishu acupoint or non-Feishu acupoint.
出处
《中成药》
CAS
CSCD
北大核心
2012年第6期1039-1044,共6页
Chinese Traditional Patent Medicine
基金
国家自然科学基金资助项目(81073066)
关键词
芥子碱
穴位
皮肤微透析
血液微透析
sinapine
acupoint
subcutaneous microdialysis
blood microdialysis
